• Title/Summary/Keyword: Inhibitory Activity

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Studies on Antioxidant, Anti-inflammation and Tyrosinase Inhibitory Activities of Melissa officinalis Extracts and Their Fractions (레몬밤 추출물과 분획물의 항산화, 항염 및 티로시나제 저해활성 연구)

  • Jeong, Yong Un;Lee, Hwan;Park, Haney;Kim, Kyungmin;Kim, Suyeong;Park, Young Jin
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.44 no.4
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    • pp.465-475
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    • 2018
  • This study was carried out to evaluate the antioxidant, anti-inflammation, and tyrosinase inhibitory activity of Melissa officinalis extracts and their fractions. The total polyphenol contents of the extracts were 33.02-302.76 mg GAE/g and total flavonoid contents were 9.98-325.07 mg CE/g. In 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, DPPH radical scavenging activity was observed in the extracts and water fractions of M. officinalis and similar to that of ascorbic acid ($30{\mu}M$). In addition, the treatment of chloroform fraction significantly inhibited the production of nitric oxide (NO) in RAW 264.7 cells, indicating that they have anti-inflammatory activity. Tyrosinase inhibitory activity of $200{\mu}g/mL$ of 100% ethanol reflux extract showed better inhibitory activity than arbutin treatment at statistically significant level. As a result, it is considered that M. officinalis can be used as an effective cosmetic ingredient having antioxidant, anti-inflammation, and whitening activity.

Quinone Reductase Inductive Activity and Growth Inhibitory Effect against Hepatoma Cell of Oriental Melon Extract (참외 추출물의 Quinone Reductase 유도활성 및 간암세포 증식 억제효과)

  • Kim, Hye-Suk;Ku, Kang-Mo;Suh, Jun-Kyu;Kang, Young-Hwa
    • Journal of Bio-Environment Control
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    • v.18 no.4
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    • pp.448-453
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    • 2009
  • This study was performed to elucidate anticancer activities of various parts, such as peel, flesh, placenta, seed, stalk and stem leaf of oriental melon. Chemopreventive and anticancer effects of oriental melon extract were evaluated by detoxifying enzyme, quinone reductase (QR) inductive activity, cytotoxicity and growth inhibitory effect against hepatoma cell. Stalk and stem leaf extracts of oriental melon showed the increment of QR inductive activity with dose-dependent manner and induced quinone reductase 3.9, 1.5-fold at $200{\mu}g/mL$ respectively compared to control. The growth inhibitory effect of oriental melon extract against mouse hepatoma cell (Hepa1c1c7) was investigated by crystal violet (CV) assay. Stalk and stem leaf of oriental melon showed potent growth inhibitory effect. Based on these result, the growth inhibitory effects of stalk, stem leaf at various concentration were examined in detail by MTT assay using human hepatoma cancer cell (HepG2). All of two parts showed growth inhibitory effects and expecially stalk exhibited inhibitory effect of 60.3% at maximum concentration. The above results suggest that stalk of oriental melon has a possibility as a source of natural cancer chemopreventive materials.

Antioxidant and α-Glucosidase Inhibitory Activities of the Extracts of Aster koraiensis Leaves (국내산 벌개미취 잎 추출물의 α-glucosidase 억제능 및 항산화 활성 평가)

  • Lee, Tae Gu;Hyun, Soo Wang;Lee, Ik Soo;Park, Bong Kyun;Kim, Jin Sook;Kim, Chan Sik
    • Korean Journal of Medicinal Crop Science
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    • v.26 no.5
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    • pp.382-390
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    • 2018
  • Background: The plant Aster koraiensis has long been used as an ingredient in folk medicine. It has been reported that Aster koraiensis extract (AKE) prevents the progression of diabetes-induced retinopathy and nephropathy. However, although these beneficial effects of AKE on diabetes complications have been identified, the antidiabetic effects of AKE have not yet been completely investigated and quantified. In the present study, the glucose-lowering and antioxidant effects of aqueous and ethanolic AKEs were evaluated. Methods and Results: The glucose-lowering effects of aqueous and ethanolic (30%-, 50%-, and 80%-ethanol) AKEs were investigated via ${\alpha}$-glucosidase inhibitory assays. The mode of inhibition by AKEs on ${\alpha}$-glucosidase was identified through kinetic analysis. The total antioxidant capacity of each of the 4 AKEs was evaluated by assessing their conversion rate of $Cu^{2+}$ to $Cu^+$. The content of chlorogenic acid and 3,5-di-O-caffeoylquinic acid, the bioactive compounds in AKE, in each extract were analyzed by high performance liquid chromatography (HPLC). The AKEs showed potent ${\alpha}$-glucosidase inhibitory activity with mixed inhibition mode, and significant antioxidant capacity. Conclusions: These results of this study suggested that the AKEs tested had ${\alpha}$-glucosidase inhibitory and antioxidant effects. Among the extracts, the 80% ethanol extract showed the most significant ${\alpha}$-glucosidase inhibitory activity, with a half maximal inhibitory concentration ($IC_{50}$ value) of $1.65{\pm}0.36mg/m{\ell}$ and a half maximal effective concentration ($EC_{50}$ value) for its antioxidant activity of $0.42{\pm}0.10mg/m{\ell}$. It can therefore be used as a source of therapeutic agents to treat diabetes patients.

Free Radical Scavenging Activities and Inhibitory Effects on Xanthine Oxidase by Ethanol Extract from Capsella bursa-pastoris (냉이(Capsella bursa-pastoris)에탄을 추출물의 유리라디칼 소거 및 Xathine Oxidase 저해활성)

  • Hong, Jung-Il;Ra, Kyung-Soo;Sung, Ha-Chin;Yang, Han-Chul;Kweon, Mee-Hyang
    • Applied Biological Chemistry
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    • v.38 no.6
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    • pp.590-595
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    • 1995
  • To examine the characteristics of antioxidative compounds from Capsella bursa-pastoris, ethanol extracts were separated into five organic solvent fractions; hexane(Fr.H), diethyl ether (Fr.E), ethyl acetate(Fr.EA), butanol (Fr.B), and water(Fr.D) fractions. Fr.B showed the greatest electron donating ability and inhibitory effect on lipid peroxidation. Whereas Fr.E had the most excellent activity in the superoxide radical scavenging activity by xanthine/xanthine oxidase-cytochrome c reduction system. The inhibitory effect of each fraction on xanthine oxidase was also measured. Fr.E had the strongest inhibitory effect on xanthine oxidase and $IC_{50}$ was $5.65\;{\mu}g$. The results indicate that the superoxide radical scavenging activity of Fr.E is caused by the inhibitory effect on radical generating system of xanthine oxidase. Also the order of inhibitory effect on xanthine oxidase was Fr.B

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Antihyperglycemic α-Glucosidase Inhibitory Activity of Ethanol Extract from Neolentinus lepideus (잣버섯(Neolentinus lepideus) 에탄올 추출물의 혈당상승 억제 효과)

  • Shin, Ja-Won;Bae, Sang-Min;Han, Sang-Min;Lee, Yun-Hae;Kim, Jeong-Han;Ji, Jeong-Hyun;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.43 no.3
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    • pp.174-179
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    • 2015
  • For development a new anti-diabetic compound from edible mushroom, antihyperglycemic ${\alpha}$-glucosidase inhibitory activities of Pleurotus ostreatus, Pleurotus cornucopiae, Pleurotus salmoneostramineus, Pleurotus eryngii and Neolentinus lepideus were investigated on its water and ethanol extracts. ${\alpha}$-Glucosidase inhibitory activity of Neolentinus lepideus fruiting body showed the highest at 86.3% in the 95% ethanol extracts and water extract from Pleurotus cornucopiae was also higher at 48.5% among water extracts. Therefore, Neolentinus lepideus which showed very high ${\alpha}$-glucosidase inhibitory activity was selected as a new anti-diabetic agent-containing mushroom and the ${\alpha}$-glucosidase inhibitor was maximally extracted when treated with 95% ethanol at $30^{\circ}C$ for 48 hr. The ethanol extracts from Neolentinus lepideus fruiting body showed dosage-dependent hypoglycemic action after administration to 120 min in the SD-rat and streptozotocin-induced diabetic SD-rat.

$\alpha$-Glucosidase and $\alpha$-Amylase Inhibitory Activity of Compounds from Roots Extract of Pueraria thunbergiana (갈근에서 분리한 화합물의 $\alpha$-glucosidase와 $\alpha$-amylase 활성 저해 효과)

  • Park, Jee-Hee;Baek, Mok-Ryeon;Lee, Byung-Hoi;Yon, Gyu-Hwan;Ryu, Shi-Yong;Kim, Young-Sup;Park, Sang-Un;Hong, Kyung-Sik
    • Korean Journal of Medicinal Crop Science
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    • v.17 no.5
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    • pp.357-362
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    • 2009
  • Compounds of isolated from roots extract of Pueraria thunbergiana were tested their inhibitory effects on $\alpha$-glucosidase and $\alpha$-amylase. Inhibitory activity of methylene chloride (MC) fraction and ethyl acetate (EA) fraction against $\alpha$-glucosidase showed more than 60% at a concentration of $500{\mu}g/m{\ell}$. Among the nine compounds tested on $\alpha$-glucosidase, biochanin A, (-)-tuberosin and calycosin from MC fraction and daidzein from EA fraction were stronger inhibitors than acarbose ($IC_{50}=530{\mu}g/m{\ell}$), and their $IC_{50}$ were 9, 144, 328 and $20{\mu}g/m{\ell}$, respectively. Biochanin A and (-)-tuberosin also inhibited $\alpha$-amylase activity as like as acarbose $IC_{50}=20.5{\mu}g/m{\ell}$), and their $IC_{50}$ were 22 and $348{\mu}g/m{\ell}$, respectively. Although daidzein was already known $\alpha$-glucosidase inhibitory effects, it was newly evaluated that biochanin A and (-)-tuberosin inhibited $\alpha$-glucosidase as well as $\alpha$-amylase, and that calycosin did $\alpha$-glucosidase.

Screening on Allogeneic Mixed Lymphocyte Culture Inhibitory Activity for the Extracts of Marine-Derived Microorganisms (해양미생물 추출물의 동종세포반응 (Allogeneic Mixed Lymphocyte Culture) 억제효능 검색)

  • Yun, Keum-Ja;Oh, Keun-Hee;Lee, Dong-Sup;Choi, Hong-Dae;Kang, Jung-Sook;Son, Byeng-Wha
    • Korean Journal of Pharmacognosy
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    • v.42 no.4
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    • pp.354-360
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    • 2011
  • In order to screen new allogeneic mixed lymphocyte culture (allo-MLR) inhibitor which is expected to be immunomodulating drug lead, we have investigated allo-MLR inhibitory activity on the marine-derived symbiotic microorganisms (1,895 strains) from the marine algae. The potent inhibitory activities (over 45% inhibition of proliferation at 10 and 2 ${\mu}g/ml$) without cytotoxicity were observed in the extracts of 46 strains. While, the significant stimulating activities (over 100% proliferation at 10 and 2 ${\mu}g/ml$) without cytotoxicity were observed in the extracts of 5 strains. In the second assay using 46 bioactive strains, 14 strains exhibited again significant allo-MLR inhibitory activity. Finally, 11 strains among the 14 strains inhibited proliferation and IFN-${\gamma}$ production of CD4+ T cells during the stimulation with specific antigen in the third assay. On the basis of above results, the marine algae is nice source for isolation of immunomodulating microorganism, and the marine algae-associated microorganism is also nice target for development of the new immunomodulating drug lead.

Effect of Clonidine on the Changes in Dorsal Horn Cell Activity Induced by Chemical Algogenics (통각유발물질에 의한 척수후각세포의 반응에 미치는 Clonidine의 영향)

  • Lee, Kwang-Hoon;Kim, Jin-Hyuk;Shin, Hong-Kee;Kim, Kee-Soon
    • The Korean Journal of Physiology
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    • v.22 no.2
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    • pp.245-257
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    • 1988
  • The present study was undertaken to investigate the effect of clonidine on the response of the dorsal horn cells to intra-arterially administered bradykinin $(BK:40{\mu}g)$ and $K^+(4mg)$ in spinal cats and cats with intact spinal cord. The change in the activities of low threshold (LT), high threshold (HT) and wide dynamic range (WDR) cells induced by BK and $K^+$ were determined before and after treatment of animals with clonidine. Also studied was mechanism of inhibitory action of clonidine on the responses of dorsal horn cells to the chemical algogenics. Number of WDR cell responded to intra-arterially administered BK and $K^+$ was greater in spinal animals than in cats with intact spinal cord. Following administration of BK or $K^+$ no change was observed in the activity of LT cell whereas activity of HT cell increased invariably. The increased response of HT cell to BK and $K^+$ was markedly suppressed by clonidine. On the other hand, such inhibitory actions of clonidine were almost completely blocked by yohimbine. The majority of WDR cells were activated by $K^+$ while response of WDR cells to BK was diverse (excitatory, inhibitory or mixed). These results indicate that clonidine inhibits responses of the dorsal horn cells not only to thermal or mechanical stimulations but also to chemical algogenics, and that the inhibitory action of clonidine is generally mediated through excitation of ${\alpha}_2-adrenoreceptors$.

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Development of Cholinesterase Inhibitors using 1-Benzyl Piperidin-4-yl (α)-Lipoic Amide Molecules

  • Lee, Seung-Hwan;Kim, Beom-Cheol;Kim, Jae-Kwan;Lee, Hye Sook;Shon, Min Young;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • v.35 no.6
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    • pp.1681-1686
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    • 2014
  • A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.

Inhibition of Monoamine Oxidase B by Cigarette Smoke Constituents

  • Lim, Heung-Bin;Sohn, Hyug-Ok;Lee, Young-Gu;Moon, Ja-Young;Kang, Young-Kook;Kim, Yong-Ha;Lee, Un-Chul;Lee, Dong-Wook
    • Journal of the Korean Society of Tobacco Science
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    • v.19 no.2
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    • pp.136-144
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    • 1997
  • Cigarette smoking is known to suppress both 1-methy14-phenyl-155,Ltetrahydropy-ridine (MPTP)-induced parkinsonism and idiopathic Parkinson's disease (PD). However, the precise mechanism underlying its protective action against PD is not clearly elucidated yet. In order to find possible clue on the mechanism of protective action of smoking, we investigated the inhibitory effect of cigarette smoke components on rat brain mitochondria1 monoamine oxidase B (MAO-B), responsible enzyme for the activation of MPTP to its toxic metabolitesr and identified the components having an inhibitory potency on this enzyme from cigarette smoke. Total 31 eligible constituents including nicotine were selected from cigarette smoke condensates via solvents partitioning and silica gel chromatographic separation, and inhibitory potencies of 19 components on MAO-B were determined. Hydroquinone and methylcatechol, the phenolic components, showed the strongest inhibitory potencies on MAO-B activity in the components tested. 3,4-Dihydroxybenzylamino, myosmine and indole in basic fracton, eugenol in phenolic fraction, and farnesol in neutral fraction also inhibited the enzyme activity dose-dependently. Among tobacco alkaloids tested only myosmine was effective for the inhibition of this enzyme. These results suggest that the decrease in MAO-B activity by such components derived from cigarette smoke seems to be related to the suppression of MPTP-induced neurotoxicity and to the less incidence of Parkinson's disease in smokers than in nonsmokers.

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